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杂环化合物(2013 - 2022年)作为多发性硬化症药物设计中有效药效基团的实验研究

Experimentation of Heterocycles (2013-22) as Potent Pharmacophores in Drug Design of Multiple Sclerosis.

作者信息

Dorababu Atukuri

机构信息

SKNG Government First Grade College, Gangavathi, 583227, Karnataka, India.

出版信息

Drug Dev Res. 2025 Feb;86(1):e70059. doi: 10.1002/ddr.70059.

DOI:10.1002/ddr.70059
PMID:39907074
Abstract

Multiple sclerosis (MS) is a demyelinating disease in which the insulating cover (myelin sheath) of the brain and spinal cord is damaged. Demyelination results in a decreased signal transmission in the nervous system. Symptoms include double vision, muscle weakness, and difficulty with coordination. Genetic and viral infections have been proposed as plausible factors responsible for MS. Although there is no cure for MS, treatment prevents future attacks. At present, chemotherapy and monoclonal antibodies are the available treatments for MS. Heterocyclic compounds are currently being tested clinically for their efficacy. Some heterocyclic scaffolds have been found to be promising for the treatment of MS. In view of this, research has been conducted towards the design and discovery of chemical agents for MS. Hence, the literature relevant to drug design for MS in the last decade has been collated and described comprehensively so that it would be helpful for efficient drug design for MS in the future. Additionally, through the structure-activity relationship, the importance of crucial structural features was emphasized. The classification was primarily based on the type of heterocycle.

摘要

多发性硬化症(MS)是一种脱髓鞘疾病,其中脑和脊髓的绝缘覆盖层(髓鞘)受损。脱髓鞘导致神经系统中的信号传递减少。症状包括复视、肌肉无力和协调困难。遗传因素和病毒感染被认为是导致MS的可能因素。虽然MS无法治愈,但治疗可预防未来的发作。目前,化疗和单克隆抗体是MS的可用治疗方法。杂环化合物目前正在进行临床疗效测试。已发现一些杂环骨架对治疗MS有前景。有鉴于此,已开展了针对MS化学药剂的设计和发现的研究。因此,对过去十年中与MS药物设计相关的文献进行了整理和全面描述,以便对未来高效的MS药物设计有所帮助。此外,通过构效关系,强调了关键结构特征的重要性。分类主要基于杂环的类型。

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